Articles & Reviews


Valderrama, K., Pradel, E., Firsov, A. M., Drobecq, H., Bauderlique-le Roy, H., Villemagne, B., Antonenko, Y. N., & Hartkoorn, R. C. Pyrrolomycins Are Potent Natural Protonophores. Antimicrob. Agents Chemother.,2019, 63(10): e01450-01419. 10.1128/AAC.01450-19

Willand, N., Flipo, M., Villemagne, B., Baulard, A., & Deprez, B. 2019. Chapter Five - Recent advances in the design of inhibitors of mycobacterial transcriptional regulators to boost thioamides anti-tubercular activity and circumvent acquired-resistance. In K. Chibale (Ed.), Annual Reports in Medicinal Chemistry, Vol. 52: 131-152: Academic Press. 10.1016/bs.armc.2019.06.003

Lagarde, N., Goldwaser, E., Pencheva, T., Jereva, D., Pajeva, I., Rey, J., Tuffery, P., Villoutreix, B. O., & Miteva, M. A. A Free Web-Based Protocol to Assist Structure-Based Virtual Screening Experiments. Int. J. Mol. Sci.,2019, 20(18): 4648.10.3390/ijms20184648

Sartori, M., Mendes, T., Desai, S., Lasorsa, A., Herledan, A., Malmanche, N., Mäkinen, P., Marttinen, M., Malki, I., Chapuis, J., Flaig, A., Vreulx, A.-C., Ciancia, M., Amouyel, P., Leroux, F., Deprez, B., Cantrelle, F.-X., Maréchal, D., Pradier, L., Hiltunen, M., Landrieu, I., Kilinc, D., Herault, Y., Laporte, J., & Lambert, J.-C. BIN1 recovers tauopathy-induced long-term memory deficits in mice and interacts with Tau through Thr348 phosphorylation. Acta Neuropathol. (Berl).2019, 138(4): 631-652.10.1007/s00401-019-02017-9

Leroux, F., Bosc, D., Beghyn, T., Hermant, P., Warenghem, S., Landry, V., Pottiez, V., Guillaume, V., Charton, J., Herledan, A., Urata, S., Liang, W., Sheng, L., Tang, W.-J., Deprez, B., & Deprez-Poulain, R. Identification of ebselen as a potent inhibitor of insulin degrading enzyme by a drug repurposing screening. Eur. J. Med. Chem.,2019, 179: 557-566.10.1016/j.ejmech.2019.06.057

Prevet, H., Moune, M., Tanina, A., Kemmer, C., Herledan, A., Frita, R., Wohlkönig, A., Bourotte, M., Villemagne, B., Leroux, F., Gitzinger, M., Baulard, A. R., Déprez, B., Wintjens, R., Willand, N., & Flipo, M. A fragment-based approach towards the discovery of N-substituted tropinones as inhibitors of Mycobacterium tuberculosis transcriptional regulator EthR2. Eur. J. Med. Chem.,2019, 167: 426-438.10.1016/j.ejmech.2019.02.023

Colin, B., Deprez, B., & Couturier, C. High-throughput DNA plasmid transfection using acoustic droplet ejection technology. SLAS Discovery,2019, 24(4): 492-500.10.1177/2472555218803064

Tanina, A., Wohlkönig, A., Soror, S. H., Flipo, M., Villemagne, B., Prevet, H., Déprez, B., Moune, M., Perée, H., Meyer, F., Baulard, A. R., Willand, N., & Wintjens, R. A comprehensive analysis of the protein-ligand interactions in crystal structures of Mycobacterium tuberculosis EthR. Biochimica et Biophysica Acta (BBA) - Proteins and Proteomics,2019, 1867(3): 248-258.10.1016/j.bbapap.2018.12.003

Colin, B., Rocq, N., Deprez, B., & Couturier, C. High-Throughput DNA Plasmid Multiplexing and Transfection Using Acoustic Nanodispensing Technology. J. Vis. Exp.,2019, 150: e59570.10.3791/59570

Machelart, A., Salzano, G., Li, X., Demars, A., Debrie, A.-S., Menendez-Miranda, M., Pancani, E., Jouny, S., Hoffmann, E., Deboosere, N., Belhaouane, I., Rouanet, C., Simar, S., Talahari, S., Giannini, V., Villemagne, B., Flipo, M., Brosch, R., Nesslany, F., Deprez, B., Muraille, E., Locht, C., Baulard, A. R., Willand, N., Majlessi, L., Gref, R., & Brodin, P. Intrinsic Antibacterial Activity of Nanoparticles Made of β-Cyclodextrins Potentiates Their Effect as Drug Nanocarriers against Tuberculosis. ACS Nano,2019, 13(4): 3992-4007.10.1021/acsnano.8b07902

Pastor, A., Machelart, A., Li, X., Willand, N., Baulard, A., Brodin, P., Gref, R., & Desmaële, D. A novel codrug made of the combination of ethionamide and its potentiating booster: synthesis, self-assembly into nanoparticles and antimycobacterial evaluation. Org. Biomol. Chem.,2019, 17(20): 5129-5137.10.1039/C9OB00680J


Colin, B., Deprez, B., & Couturier, C. High-throughput DNA plasmid transfection using acoustic droplet ejection technology. SLAS Discovery,2018: in press. 10.1177/2472555218803064

Prieri, M., Frita, R., Probst, N., Sournia-Saquet, A., Bourotte, M., Déprez, B., Baulard, A. R., & Willand, N. Efficient analoging around ethionamide to explore thioamides bioactivation pathways triggered by boosters in Mycobacterium tuberculosis. Eur. J. Med. Chem.,2018, 159: 35-46.10.1016/j.ejmech.2018.09.038

Zhang, Z., Liang, W. G., Bailey, L. J., Tan, Y. Z., Wei, H., Wang, A., Farcasanu, M., Woods, V. A., McCord, L. A., Lee, D., Shang, W., Deprez-Poulain, R., Deprez, B., Liu, D. R., Koide, A., Koide, S., Kossiakoff, A. A., Li, S., Carragher, B., Potter, C. S., & Tang, W.-J. Ensemble cryoEM elucidates the mechanism of insulin capture and degradation by human insulin degrading enzyme. eLife,2018, 7: e33572. 10.7554/eLife.33572

Hoguet, V., Charton, J., Hecquet, P.-E., Lakhmi, C., & Lipka, E. Supercritical fluid chromatography versus high performance liquid chromatography for enantiomeric and diastereoisomeric separations on coated polysaccharides-based stationary phases: Application to dihydropyridone derivatives. J. Chromatogr. A,2018, 1549: 39-50.10.1016/j.chroma.2018.03.035

Kussau, T., Flipo, M., Van Wyk, N., Viljoen, A., Olieric, V., Kremer, L., & Blaise, M. Structural rearrangements occurring upon cofactor binding in the Mycobacterium smegmatis beta-ketoacyl-acyl carrier protein reductase MabA. Acta crystallographica. Section D, Structural biology,2018, 74(Pt 5): 383-393. 10.1107/s2059798318002917

Hering, Y., Berthier, A., Duez, H., Lefebvre, P., Deprez, B., Gribbon, P., Wolf, M., Reinshagen, J., Halley, F., Hannemann, J., Böger, R., Staels, B., & Gul, S. Development and implementation of a cell-based assay to discover agonists of the nuclear receptor REV-ERBα. 2018,2018. 10.14440/jbm.2018.244


Wohlkönig, A., Remaut, H., Moune, M., Tanina, A., Meyer, F., Desroses, M., Steyaert, J., Willand, N., Baulard, A. R., & Wintjens, R. Structural analysis of the interaction between spiroisoxazoline SMARt-420 and the Mycobacterium tuberculosis repressor EthR2. Biochem. Biophys. Res. Commun.,2017, 487(2): 403-408.10.1016/j.bbrc.2017.04.074

Tatum, N. J., Liebeschuetz, J. W., Cole, J. C., Frita, R., Herledan, A., Baulard, A. R., Willand, N., & Pohl, E. New active leads for tuberculosis booster drugs by structure-based drug discovery. Org. Biomol. Chem.,2017, 15(48): 10245-10255.10.1039/C7OB00910K

Salzano, G., Wankar, J., Ottani, S., Villemagne, B., Baulard, A. R., Willand, N., Brodin, P., Manet, I., & Gref, R. Cyclodextrin-based nanocarriers containing a synergic drug combination: A potential formulation for pulmonary administration of antitubercular drugs. Int. J. Pharm.,2017, 531(2): 577-587.10.1016/j.ijpharm.2017.05.030

Montaigne, D., Marechal, X., Modine, T., Coisne, A., Mouton, S., Fayad, G., Ninni, S., Klein, C., Ortmans, S., Seunes, C., Potelle, C., Berthier, A., Gheeraert, C., Piveteau, C., Deprez-Poulain, R., Eeckhoute, J., Duez, H., Lacroix, D., Deprez, B., Jegou, B., Koussa, M., Edme, J. L., Lefebvre, P., & Staels, B. Daytime variation of perioperative myocardial injury in cardiac surgery and its prevention by Rev-Erbalpha antagonism: a single-centre propensity-matched cohort study and a randomised study. Lancet,2017 391(10115): 59–69 .10.1016/s0140-6736(17)32132-3

Hermant, P., Bosc, D., Piveteau, C., Gealageas, R., Lam, B. V., Ronco, C., Roignant, M., Tolajanahary, H., Jean, L., Renard, P.-Y., Lemdani, M., Bourotte, M., Herledan, A., Bedart, C., Biela, A., Leroux, F., Deprez, B., & Deprez-Poulain, R. Controlling Plasma Stability of Hydroxamic Acids: A MedChem Toolbox. Journal of Medicinal Chemistry,2017, 60(21): 9067–9089. 10.1021/acs.jmedchem.7b01444

Costa-Gouveia, J., Pancani , E., Jouny, S., Machelart, A., Delorme, V., Salzano, G., Iantomasi, R., Piveteau, C., Queval, C., Song, O.-R., Flipo, M., Deprez, B., Saint-André, J.-P., Hureaux, J., Majlessi, L., Willand, N., Baulard, A., Brodin, P., & Gref, R. Combination therapy for tuberculosis treatment: pulmonary administration of ethionamide and booster co-loaded nanoparticles. Scientific Reports,2017, 7: Article number: 5390 10.1038/s41598-017-05453-3

Dequirez, G., Bourotte, M., Porras de Francisco, E., Remuiñan, Blanco, M. J., Deprez, B., & Willand, N. Microwave-Assisted Suzuki-Miyaura Cross Coupling using Nickel as Catalyst to Rapidly Access to 3-Arylazetidine. ChemistrySelect,2017, 2(28): 8841-8846.10.1002/slct.201702101. 10.1002/slct.201702101

Boiteau, J.-G., Ouvry, G., Arlabosse, J.-M., Astri, S., Beillard, A., Bhurruth-Alcor, Y., Bonnary, L., Bouix-Peter, C., Bouquet, K., Bourotte, M., Cardinaud, I., Comino, C., Deprez, B., Duvert, D., Féret, A., Hacini-Rachinel, F., Harris, C. S., Luzy, A.-P., Mathieu, A., Millois, C., Orsini, N., Pascau, J., Pinto, A., Piwnica, D., Polge, G., Reitz, A., Reversé, K., Rodeville, N., Rossio, P., Spiesse, D., Tabet, S., Taquet, N., Tomas, L., Vial, E., & Hennequin, L. F. Discovery and process development of a novel TACE inhibitor for the topical treatment of psoriasis. Bioorganic & Medicinal Chemistry,2017: in press. 10.1016/j.bmc.2017.07.054

Lasalle, M., Hoguet, V., Hennuyer, N., Leroux, F., Piveteau, C., Belloy, L., Lestavel, S., Vallez, E., Dorchies, E., Duplan, I., Sevin, E., Culot, M., Gosselet, F., Boulahjar, R., Herledan, A., Staels, B., Deprez, B., Tailleux, A., & Charton, J. Topical Intestinal Aminoimidazole Agonists of G-Protein-Coupled Bile Acid Receptor 1 Promote Glucagon Like Peptide-1 Secretion and Improve Glucose Tolerance. Journal of Medicinal Chemistry,2017, 60(10): 4185-4211. 10.1021/acs.jmedchem.6b01873

Delplanques, T., Boulahjar, R., Charton, J., Houze, C., Howsam, M., Servais, A.-C., Fillet, M., & Lipka, E. Single and dual cyclodextrins systems for the enantiomeric and diastereoisomeric separations of structurally related dihydropyridone analogues. Electrophoresis 2017, 38(15): 1922-1931.10.1002/elps.201600536

Blondiaux, N., Moune, M., Desroses, M., Frita, R., Flipo, M., Mathys, V., Soetaert, K., Kiass, M., Delorme, V., Djaout, K., Trebosc, V., Kemmer, C., Wintjens, R., Wohlkönig, A., Antoine, R., Huot, L., Hot, D., Coscolla, M., Feldmann, J., Gagneux, S., Locht, C., Brodin, P., Gitzinger, M., Déprez, B., Willand, N., & Baulard, A. R. Reversion of antibiotic resistance in Mycobacterium tuberculosis by spiroisoxazoline SMARt-420. Science,2017, 355(6330): 1206-1211. doi:10.1126/science.aag1006

Wohlkönig, A., Remaut, H., Moune, M., Tanina, A., Meyer, F., Desroses, M., Steyaert, J., Willand, N., Baulard, A. R., & Wintjens, R. Structural analysis of the interaction between spiroisoxazoline SMARt-420 and the Mycobacterium tuberculosis repressor EthR2. Biochemical and Biophysical Research Communications,2017, 487(2): 403-408.doi:10.1016/j.bbrc.2017.04.074

Mpakali, A., Giastas, P., Deprez-Poulain, R., Papakyriakou, A., Koumantou, D., Gealageas, R., Tsoukalidou, S., Vourloumis, D., Mavridis, I. M., Stratikos, E., & Saridakis, E. Crystal Structures of ERAP2 Complexed with Inhibitors Reveal Pharmacophore Requirements for Optimizing Inhibitor Potency. ACS Medicinal Chemistry Letters,2017, 8(3): 333-337.doi:10.1021/acsmedchemlett.6b00505

Ouvry, G., Berton, Y., Bhurruth-Alcor, Y., Bonnary, L., Bouix-Peter, C., Bouquet, K., Bourotte, M., Chambon, S., Comino, C., Deprez, B., Duvert, D., Duvert, G., Hacini-Rachinel, F., Harris, C. S., Luzy, A.-P., Mathieu, A., Millois, C., Pascau, J., Pinto, A., Polge, G., Reitz, A., Reversé, K., Rosignoli, C., Taquet, N., & Hennequin, L. F. Identification of novel TACE inhibitors compatible with topical application. 2017 Bioorganic & Medicinal Chemistry Letters,in press.doi:10.1016/j.bmcl.2017.02.035


Chapuis, J., Flaig, A., Grenier-Boley, B., Eysert, F., Pottiez, V., Deloison, G., Vandeputte, A., Ayral, A.-M., Mendes, T., Desai, S., Goate, A. M., Kauwe, J. S. K., Leroux, F., Herledan, A., Demiautte, F., Bauer, C., Checler, F., Petersen, R. C., Blennow, K., Zetterberg, H., Minthon, L., Van Deerlin, V. M., Lee, V. M.-Y., Shaw, L. M., Trojanowski, J. Q., Albert, M., Moghekar, A., O’Brien, R., Peskind, E. R., Malmanche, N., Schellenberg, G. D., Dourlen, P., Song, O.-R., Cruchaga, C., Amouyel, P., Deprez, B., Brodin, P., & Lambert, J.-C. Genome-wide, high-content siRNA screening identifies the Alzheimer’s genetic risk factor FERMT2 as a major modulator of APP metabolism. Acta Neuropathologica,2016. doi:1-12.10.1007/s00401-016-1652-z

Bauters, D., Scroyen, I., Deprez-Poulain, R., & Lijnen, H. R. ADAMTS5 promotes murine adipogenesis and visceral adipose tissue expansion. Thromb Haemost,2016, 116(4). doi:10.1160/th16-01-0015

Prevet, H., Flipo, M., Roussel, P., Deprez, B., & Willand, N. Microwave-assisted synthesis of functionalized spirohydantoins as 3-D privileged fragments for scouting the chemical space. Tetrahedron Letters,2016, 57(26): 2888-2894.doi:10.1016/j.tetlet.2016.05.065

Letronne, F., Laumet, G., Ayral, A. M., Chapuis, J., Demiautte, F., Laga, M., Vandenberghe, M. E., Malmanche, N., Leroux, F., Eysert, F., Sottejeau, Y., Chami, L., Flaig, A., Bauer, C., Dourlen, P., Lesaffre, M., Delay, C., Huot, L., Dumont, J., Werkmeister, E., Lafont, F., Mendes, T., Hansmannel, F., Dermaut, B., Deprez, B., Herard, A. S., Dhenain, M., Souedet, N., Pasquier, F., Tulasne, D., Berr, C., Hauw, J. J., Lemoine, Y., Amouyel, P., Mann, D., Deprez-Poulain, R., Checler, F., Hot, D., Delzescaux, T., Gevaert, K., & Lambert, J. C. ADAM30 Downregulates APP-Linked Defects Through Cathepsin D Activation in Alzheimer's Disease. EBioMedicine,2016: in press. doi:10.1016/j.ebiom.2016.06.002 OPEN ACCESS

Probst, N. P., Deprez, B., & Willand, N. Palladium-free Sonogashira-type cross-coupling reaction of bromoisoxazolines or N-alkoxyimidoyl bromides and alkynes. Tetrahedron Letters,2016, 57(10): 1066-1070. doi:10.1016/j.tetlet.2016.01.070

Bosc, D., Jakhlal, J., Deprez, B., & Deprez-Poulain, R. Kinetic target-guided synthesis in drug discovery and chemical biology: a comprehensive facts and figures survey. Future Medicinal Chemistry,2016: in press. doi:10.4155/fmc-2015-0007 OPEN ACCESS


Broeders, E. M., Nascimento, E. M., Havekes, B., Brans, B., Roumans, K. M., Tailleux, A., Schaart, G., Kouach, M., Charton, J., Deprez, B., Bouvy, N., Mottaghy, F., Staels, B., van Marken Lichtenbelt, W. D., & Schrauwen, P. The Bile Acid Chenodeoxycholic Acid Increases Human Brown Adipose Tissue Activity. Cell Metabolism,2015, 22(3): 418-426. doi:10.1016/j.cmet.2015.07.002

Deprez-Poulain, R., Nathalie, H., Bosc, D., Liang, W. G., Enee, E., Marechal, X., Julie, C., Totobenazara, J., Berte, G., Jahklal, J., Verdelet, T., Dumont, J., Dassonneville, S., Woitrain, E., Gauriot, M., Paquet, C., Duplan, I., Hermant, P., Cantrelle, F.-X., Sevin, E., Culot, M., Landry, V., Herledan, A., Piveteau, C., Lippens, G., Florence, L., Tang, W. J., Van Endert, P., Staels, B., & Deprez, B. Catalytic site inhibition of insulin-degrading enzyme by a small molecule induces glucose intolerance in mice. Nature Communications,2015, 6. doi:10.1038/ncomms9250 OPEN ACCESS

Henninot, A., Terrier, A., Charton, J., Urbain, R., Fontayne, A., Deprez, B., & Beghyn, T. Characterization of monoclonal antibodies by a fast and easy LC- MS ToF analysis on culture supernatant. Analytical Biochemistry,2015: in press. doi:10.1016/j.ab.2015.08.006

Tran, N. C., Dhondt, H., Flipo, M., Deprez, B., & Willand, N. Synthesis of functionalized 2-isoxazolines as three-dimensional fragments for fragment-based drug discovery. Tetrahedron Letters,2015, 56(27): 4119-4123. doi:10.1016/j.tetlet.2015.05.035

Bonner, C., Kerr-Conte, J., Gmyr, V., Queniat, G., Moerman, E., Thevenet, J., NBeaucamps, C., Delalleau, N., Popescu, I., Malaisse, W., Sener, A., Deprez, B., Abderrahmani, A., Staels, B., & Pattou, F. Inhibition of the glucose transporter SGLT2 with dapagliflozin in pancreatic alpha cells triggers glucagon secretion. Nature Medicine,2015, 21: 512-517. doi:10.1038/nm.3828

Lasalle, M., Picon, S., Boulahjar, R., Hoguet, V., Van Obbergen, J., Roussel, P., Deprez, B., & Charton, J. Access to newly functionalized imidazole derivatives: efficient synthesis of novel 5-amino-2-thioimidazoles using propylphosphonic anhydride (®T3P). Tetrahedron Letters,2015, 56(8): 1011-1014. doi:10.1016/j.tetlet.2015.01.046

Charton, J., Gauriot, M., Totobenazara, J., Hennuyer, N., Dumont, J., Bosc, D., Marechal, X., Elbakali, J., Herledan, A., Wen, X., Ronco, C., Gras-Masse, H., Heninot, A., Pottiez, V., Landry, V., Staels, B., Liang, W. G., Leroux, F., Tang, W. J., Deprez, B., & Deprez-Poulain, R. Structure-activity relationships of Imidazole-derived 2-[N-carbamoylmethyl-alkylamino]acetic acids, dual binders of human Insulin-Degrading Enzyme. Eur J Med Chem. 90: 547-567 doi:10.1016/j.ejmech.2014.12.005

Corbel, C., Zhang, B., Le Parc, A., Baratte, B., Colas, P., Couturier, C., Kosik, K. S., Landrieu, I., Le Tilly, V., & Bach, S. Tamoxifen Inhibits CDK5 Kinase Activity by Interacting with p35/p25 and Modulates the Pattern of Tau Phosphorylation. Chemistry & Biology,2015, 22(4): 482.doi:10.1016/j.chembiol.2015.03.009

Karrout, Y., Dubuquoy, L., Piveteau, C., Siepmann, F., Moussa, E., Wils, D., Beghyn, T., Neut, C., Flament, M. P., Guerin-Deremaux, L., Dubreuil, L., Deprez, B., Desreumaux, P., & Siepmann, J. In vivo efficacy of microbiota-sensitive coatings for colon targeting: A promising tool for IBD therapy. Journal of Controlled Release,2015, 197: 121-130. doi: 10.1016/ j.jconrel. 2014.11.006


Elbakali, J., Gras, H., Maingot, L., Deprez, B., Dumont, J., Leroux, F., & Deprez-Poulain, R. Inhibition of aggrecanase as a therapeutic strategy in osteoarthritis. Future Medicinal Chemistry,2014, 6(12): 1399-1412. 10.4155/FMC.14.84

Mathieu, A. L., Sperandio, O., Pottiez, V., Balzarin, S., Herledan, A., Elkaim, J. O., Fogeron, M. L., Piveteau, C., Dassonneville, S., Deprez, B., Villoutreix, B. O., Bonnefoy, N., & Leroux, F. Identification of Small Inhibitory Molecules Targeting the Bfl-1 Anti-Apoptotic Protein That Alleviates Resistance to ABT-737. J Biomol Screen,2014, 19(7): 1035-1046. 10.1177/1087057114534070

Villemagne, B., Flipo, M., Blondiaux, N., Crauste, C., Malaquin, S., Leroux, F., Piveteau, C., Villeret, V., Brodin, P., Villoutreix, B. O., Sperandio, O., Soror, S. H., Wohlkonig, A., Wintjens, R., Deprez, B., Baulard, A. R., & Willand, N. Ligand efficiency driven design of new inhibitors of Mycobacterium tuberculosis transcriptional repressor EthR using fragment growing, merging and linking approaches. Journal of Medicinal Chemistry,2014 57(11): 4876-4888.10.1021/jm500422b

Charton, J., Gauriot, M., Guo, Q., Hennuyer, N., Marechal, X., Dumont, J., Hamdane, M., Pottiez, V., Landry, V., Sperandio, O., Flipo, M., Buee, L., Staels, B., Leroux, F., Tang, W.-J., Deprez, B., & Deprez-Poulain, R. Imidazole-derived 2-[N-carbamoylmethyl-alkylamino]acetic acids, substrate-dependent modulators of insulin-degrading enzyme in amyloid-b hydrolysis. European Journal of Medicinal Chemistry,2014, 79, 184-193.10.1016/j.ejmech.2014.04.009

Crauste, C., Willand, N., Villemagne, B., Flipo, M., Willery, E., Carette, X., Moune Dimala, M., Drucbert, A. S., Danze, P. M., Deprez, B., & Baulard, A. Unconventional Surface Plasmon Resonance signals reveal quantitative inhibition of transcriptional repressor EthR by synthetic ligands. Analytical Biochemistry,2014, 452: 54-66. 10.1016/j.ab.2014.02.011


Couturier, C., & Deprez, B. Setting up a Bioluminescence Resonance Energy Transfer high throughput screening assay to search for protein/protein interaction inhibitors in mammalian cells. Frontiers in Endocrinology,2013, 3: 100.10.3389/fendo.2012.00100

Tatum, N. J., Villemagne, B., Willand, N., Deprez, B., Liebeschuetz, J. W., Baulard, A. R., & Pohl, E. Structural and docking studies of potent ethionamide boosters. Acta Crystallographica Section C,2013, 69(11): 1243-1250.doi:10.1107/S0108270113028126

Maingot, L., Elbakali, J., Dumont, J., Bosc, D., Cousaert, N., Urban, A., Deglane, G., Villoutreix, B., Nagase, H., Sperandio, O., Leroux, F., Deprez, B., & Deprez-Poulain, R. Aggrecanase-2 Inhibitors Based on the Acylthiosemicarbazide Zinc-Binding Group. Eur J Med Chem,2013, 69: 244-261.doi: 10.1016/j.ejmech.2013.08.027

Wieniewski, K., Finnman, J., Flipo, M., Galyean, R., & Schteingart, C. D. On the mechanism of degradation of oxytocin and its analogues in aqueous solution. Biopolymers (Peptide Science),2013, 100(4): 408–421.doi: 10.1002/bip.22260

Malaquin, S., Jida, M., Courtin, J., Laconde, G., Willand, N., Deprez, B., & Deprez-Poulain, R. Water-based conditions for the microscale parallel synthesis of bicyclic lactams. Tetrahedron Letters,2013, 54(6): 562-567. doi:10.1016/j.tetlet.2012.11.082


Deprez-Poulain, R., Flipo, M., Piveteau, C., Leroux, F., Dassonneville, S., Florent, I., Maes, L., Cos, P., & Deprez, B. Structure-Activity Relationships and Blood Distribution of Antiplasmodial Aminopeptidase-1 Inhibitors. Journal of Medicinal Chemistry,2012, 55(24): 10909. doi: 10.1021/jm301506h

Deprez, B. Sciences chimiques et sciences de la vie: une coalescence prometteuse pour la pharmacie. L'actualité chimique,2012, 369: 5-7.

Gonzalez, S., Beghyn, T., Jia, J., Debreuck, N., Berte, G., Mamchaoui, K., Mouly, V., Gruenert, D., Deprez, B., & Lejeune, F. Rescue of nonsense mutations by amlexanox in human cells. Orphanet Journal of Rare Diseases,2012, 7(1): 58. doi:10.1186/1750-1172-7-58

Jida, M., Laconde, G., Soueidan, O.-M., Lebegue, N., Revelant, G., Pelinski, L., Agbossou-Niedercorn, F., Deprez, B., & Deprez-Poulain, R. Stereoselective synthesis of enantiopure N-protected-3-arylpiperazines from keto-esters. Tetrahedron Letters,2012, 53(39) 5215–5218. doi: 10.1016/j.tetlet.2012.07.031

Flipo, M., Willand, N., Lecat-Guillet, N., Hounsou, C., Desroses, M., Leroux, F., Lens, Z., Villeret, V., Wohlkönig, A., Wintjens, R., Christophe, T., Jeon, H. K., Locht, C., Brodin, P., Baulard, A., & Deprez, B. Discovery of novel N-phenyl-phenoxyacetamide derivatives as EthR inhibitors and ethionamide boosters by combining High-Throughput Screening and Synthesis. Journal of Medicinal Chemistry,2012, 55(14): 6391–6402. doi:10.1021/jm300377g

Elbakali, J., Maingot, L., Dumont, J., Host, H., Hocine, A., Cousaert, N., Dassonneville, S., Leroux, F., Deprez, B., & Deprez-Poulain, R. Novel Selective Inhibitors of Neutral Endopeptidase: Discovery by Screening and Hit-to-Lead Optimisation. Med.Chem.Comm.,2012, 3: 469-474.. doi:10.1039/C2MD00287F

Villemagne, B., Crauste, C., Flipo, M., Baulard, A. R., Deprez, B., & Willand, N. Tuberculosis: The drug development pipeline at a glance. European Journal of Medicinal Chemistry,2012, 51: 1–16. doi: 10.1016/j.ejmech.2012.02.033

Wen, X., Bakali, J. E., Deprez-Poulain, R., & Deprez, B. Efficient propylphosphonic anhydride (®T3P) mediated synthesis of benzothiazoles, benzoxazoles and benzimidazoles. Tetrahedron Letters,2012, 53(19): 2440-2443 doi:10.1016/j.tetlet.2012.03.007

Carette, X., Blondiaux, N., Willery, E., Hoos, S., Lecat-Guillet, N., Lens, Z., Wohlkonig, A., Wintjens, R., Soror, S., Frenois, F., Dirié, B., Villeret, V., England, P., Lippens, G., Deprez, B., Locht, C., Willand, N., & Baulard, A. Structural activation of the transcriptional repressor EthR from M.tuberculosis by single amino-acid change mimicking natural and synthetic ligands. Nucleic Acids Res,2012, 40(7): 3018-3030. doi: 10.1093/nar/gkr1113

Flipo, M., Desroses, M., Lecat-Guillet, N., Villemagne, B., Blondiaux, N., Leroux, F., Piveteau, C., Mathys, V., Flament, M.-P., Siepmann, J., Villeret, V., Wohlkönig, A., Wintjens, R., Soror, S. H., Christophe, T., Jeon, H. K., Locht, C., Brodin, P., Deprez, B., Baulard, A. R., & Willand, N. Ethionamide Boosters. 2. Combining Bioisosteric Replacement and Structure-Based Drug Design To Solve Pharmacokinetic Issues in a Series of Potent 1,2,4-Oxadiazole EthR Inhibitors. Journal of Medicinal Chemistry,2012, 55(1): 68-83.doi: 10.1021/jm200825u

Beghyn, T., Julie, C., Leroux, F., Henninot, A., Reboule, I., Cos, P., Maes, L., & Deprez, B. P. Drug-to-Genome-to-Drug, Step 2: Reversing Selectivity in a Series of Antiplasmodial Compounds. Journal of Medicinal Chemistry,2012, 55(3): 1274-1286 doi: 10.1021/jm201422e

Aknin, K., Gauriot, M., Totobenazara, J., Deguine, N., Deprez-Poulain, R., Deprez, B., & Charton, J. Squaric acid is a suitable building-block in 4C-Ugi reaction: access to original bivalent compounds. Tetrahedron Letters,2012, 53: 458-461. doi:10.1016/j.tetlet.2011.11.077


Grellier, E., Lecolle, K., Rogee, S., Couturier, C., D'Halluin, J.-C., Hong, S.-S., Fender, P., Boulanger, P., Quesnel, B., & Colin, M. A fiber-modified adenoviral vector interacts with immunoevasion molecules of the B7 family at the surface of murine leukemia cells derived from dormant tumors. Molecular Cancer,2011, 10(1): 105. doi: 10.1186/1476-4598-10-105

Soueidan, M., Jida, M., Bousquet, T., Niedercorn, F. A., & Pelinski, L. Efficient access to new chiral ferrocenyl [gamma]-lactams from amino alcohols. New Journal of Chemistry,2011, 35(5): 991-993. doi: 10.1039/C1NJ20059C

Bousquet, T., Jida, M., Soueidan, M., Deprez-Poulain, R., Agbossou-Niedercorn, F., & Pelinski, L. Fast and Efficient solvent-free Passerini reaction. Tetrahedron Letters,2011: in press. doi:10.1016/j.tetlet.2011.11.028

Deprez-Poulain, R., Cousaert, N., Toto, P., Willand, N., & Deprez, B. Application of Ullmann and Ullmann-Finkelstein reactions for the synthesis of N-aryl-N-(1H-pyrazol-3-yl) acetamide or N-(1-aryl-1H-pyrazol-3-yl) acetamide derivatives and pharmacological evaluation. Eur J Med Chem,2011, 46: 3867-3876. doi:10.1016/j.ejmech.2011.05.056

Soueidan, M., Jida, M., Bousquet, T., Niedercorn, F. A., & Pelinski, L. Efficient access to new chiral ferrocenyl [gamma]-lactams from amino alcohols. New Journal of Chemistry,2011, 35(5): 991-993. doi: 10.1039/C1NJ20059C

Zhang, B., Corbel, C., Gueritte, F., Couturier, C., Bach, S., & Tan, V. An in silico approach for the discovery of CDK5/p25 interaction inhibitors. Biotechnol J.,2011: in press. doi: 10.1002/biot.201100139

Bonnel, D., Legouffe, R., Willand, N., Baulard, A., Hamm, G., Deprez, B., & Stauber, J. MALDI imaging techniques dedicated to drug-distribution studies. Bioanalysis,2011, 3(12): 1399-1406. doi: 10.4155/bio.11.88

Corbel, C., Wang, Q., Bousserouel, H., Hamdi, A., Zhang, B., Lozach, O., Ferandin, Y., Tan, V., Gueritte, F., Colas, P., Couturier, C., & Bach, S. First BRET-based screening assay performed in budding yeast leads to the discovery of CDK5/p25 interaction inhibitors. Biotechnol J.,2011: in press. doi: 10.1002/biot.201100138

Seron, K., Couturier, C., Belouzard, S., Bacart, J., Monte, D., Corset, L., Bocquet, O., Dam, J., Vauthier, V., Lec Oelig Ur, C., Bailleul, B., Hoflack, B., Froguel, P., Jockers, R., & Rouille, Y. Endospanins regulate a postinternalization step of the leptin receptor endocytic pathway. Journal of Biological Chemistry,2011, (286): 17968-17981.

Flipo, M., Desroses, M., Lecat-Guillet, N., Dirié, B., Carette, X., Leroux, F., Piveteau, C., Demirkaya, F., Lens, Z., Rucktooa, P., Villeret, V., Christophe, T., Jeon, H. K., Locht, C., Brodin, P., Déprez, B., Baulard, A. R., & Willand, N. Ethionamide Boosters: Synthesis, Biological Activity, and Structure-Activity Relationships of a Series of 1,2,4-Oxadiazole EthR Inhibitors. Journal of Medicinal Chemistry,2011, 54(8): 2994-3010. doi:10.1021/jm200076a

Beghyn, T. B., Charton, J., Leroux, F., Laconde, G., Bourin, A., Cos, P., Maes, L., & Deprez, B. Drug to Genome to Drug: Discovery of New Antiplasmodial Compounds. Journal of Medicinal Chemistry,2011, 54(9): 3222–3240. doi:10.1021/jm1014617

Jida, M., Soueidan, M., Willand, N., Agbossou-Niedercorn, F., Pelinski, L., Laconde, G., Deprez-Poulain, R., & Deprez, B. A facile and rapid synthesis of N-benzyl-2-substituted piperazines. Tetrahedron Letters,2011, 52(14): 1705-1708. doi:10.1016/j.tetlet.2011.02.011


Willand, N., Desroses, M., Toto, P., Dirie, B., Lens, Z., Villeret, V., Rucktooa, P., Locht, C., Baulard, A., & Deprez, B. Exploring Drug Target Flexibility Using in Situ Click Chemistry: Application to a Mycobacterial Transcriptional Regulator. ACS Chemical Biology,2010, 5(11): 1007–1013. doi:10.1021/cb100177g

Maingot, L., Leroux, F., Landry, V., Dumont, J., Nagase, H., Villoutreix, B., Sperandio, O., Deprez-Poulain, R., & Deprez, B. New non-hydroxamic ADAMTS-5 inhibitors based on the 1,2,4-triazole-3-thiol scaffold. Bioorganic & Medicinal Chemistry Letters,2010, 21: 6213-6216. doi:10.1016/j.bmcl.2010.08.108

Jida, M., Malaquin, S., Deprez-Poulain, R., Laconde, G., & Deprez, B. Synthesis of five- and six-membered lactams via solvent-free microwave Ugi reaction. Tetrahedron Letters,2010, 51(39): 5109-5111. doi:10.1016/j.tetlet.2010.07.021

Lipka, E., Folly-Klana, M., Charton, J., Vaccher, M.-P., Bonte, J.-P., & Vaccher, C. Determination of pKa values of benzimidazole derivatives from mobility obtained by capillary electrophoresis. Journal of Pharmaceutical and Biomedical Analysis,2010, 53: 1267-1271. doi:10.1016/j.jpba.2010.07.023

Malaquin, S., Jida, M., Gesquiere, J.-C., Deprez-Poulain, R., Deprez, B., & Laconde, G. Ugi reaction for the synthesis of 4-aminopiperidine-4-carboxylic acid derivatives. Application to the synthesis of carfentanil and remifentanil. Tetrahedron Letters,2010, 51(22): 2983-2985. doi:10.1016/j.tetlet.2010.03.120

Jida, M., Deprez-Poulain, R., Malaquin, S., Roussel, P., Agbossou-Niedercorn, F., Deprez, B., & Laconde, G. Solvent-free microwave-assisted Meyers’ lactamization. Green Chemistry,2010, 12: 961 - 964. doi:10.1039/B924111F

Reynes, C., Host, H., Camproux, A.-C., Laconde, G., Leroux, F., Mazars, A., Deprez, B., Fahraeus, R., Villoutreix, B. O., & Sperandio, O. Designing Focused Chemical Libraries Enriched in Protein-Protein Interaction Inhibitors using Machine-Learning Methods. Plos Computational Biology,2010, 6(3): e1000695. doi:10.1371/journal.pcbi.1000695


Flipo, M., Charton, J., Hocine, A., Dassonneville, S., Deprez, B., & Deprez-Poulain, R. Hydroxamates: Relationships between structure and plasma-stability. J Med Chem,2009, 52(21): 6790-6802. doi:10.1021/jm900648x

Willand, N., Dirié, B., Carette, X., Bifani, P., Singhal, A., Desroses, M., Leroux, F., Déprez-Poulain, R., Frénois, F., Aumercier, M., Locht, C., Villeret, V., Déprez, B., & Baulard, A. Synthetic EthR inhibitors boost anti-tuberculous activity of ethionamide. Nature Medicine,2009, 15: 537-544.doi:10.1038/nm.1950

Charton, J., Deprez-Poulain, R., Hennuyer, N., Tailleux, A., Staels, B., & Deprez, B. Novel non-carboxylic acid retinoids: 1,2,4-Oxadiazol-5-one derivatives. Bioorganic & Medicinal Chemistry Letters,2009, 19(2): 489-492.doi:10.1016/j.bmcl.2008.11.040

Klose, D., Laprais, M., Leroux, V., Siepmann, F., Deprez, B., Bordet, R., & Siepmann, J. Fenofibrate-loaded PLGA microparticles: Effects on ischemic stroke. European Journal of Pharmaceutical Sciences,2009, 1:43-52. doi:10.1016/j.ejps.2008.12.016


Beghyn, T., Deprez-Poulain, R., Willand, N., Foleas, B., & Deprez, B. Natural compounds: leads or ideas? Bioinspired molecules for drug discovery. Chemical Biology and Drug Design,2008, 72: 3-15. doi:10.1111/j.1747-0285.2008.00673.x

Charton, J., Charruault, L., Deprez-Poulain, R., & Deprez, B. Alkylsquarates as key intermediates for the rapid preparation of original drug-inspired compounds. Combinatorial Chemistry and High Throughput Screening,2008, 11(4): 294-303.

Charton, J., Leroux, F., Delaroche, S., Landry, V., Deprez, B. P., & Deprez-Poulain, R. F. Synthesis of a Library of 200-Member Squaric Acid N-Hydroxylamide Amides. Bioorganic & Medicinal Chemistry Letters,2008, 18(18): 4968-4971. doi:10.1016/j.bmcl.2008.08.025

Cousaert, N., Willand, N., Gesquiere, J.-C., Tartar, A., Deprez, B., & Deprez-Poulain, R. Original loading and Suzuki conditions for the solid-phase synthesis of biphenyltetrazoles. Application to the first solid-phase synthesis of irbesartan. Tetrahedron Letters,2008, 49: 2743-2747. doi:10.1016/j.tetlet.2008.02.147

Vaccher, M.-P., Charton, J., Guelzim, A., Caignard, D.-H., Bonte, J.-P., & Vaccher, C.
Preparative Enantiomeric Separation of Potent AMP-Activated Protein Kinase Activator by HPLC on Amylose-Based Chiral Stationary Phase. Determination of Enantiomeric Purity and Assignment of Absolute Configuration.
Journal of Pharmaceutical and Biomedical Analysis,2008, 46(5): 920-928.

Villoutreix, B. O., Bastard, K., Sperandio, O., Fahraeus, R., Poyet, J. L., Calvo, F., Deprez, B., & Miteva, M. A.
In silico-in vitro screening of protein-protein interactions: towards the next generation of therapeutics.
Current Pharmaceutical Biotechnology,2008, 9(2): 103-122.


Beghyn, T., Deprez-Poulain, R. F., & Willand, N.
Drug Discovery and Selection - 43rd Rencontres Internationales de Chimie Thérapeutique, Lille, France.
IDDB Meeting Report ,2007.

Beghyn, T., Hounsou, C., & Deprez, B. P. PDE5 inhibitors: An original access to novel potent arylated analogues of tadalafil.
Bioorganic & Medicinal Chemistry Letters,2007, 17(3): 789-792. doi:10.1016/j.bmcl.2006.10.069

Charton, J., Cousaert, N., Bochu, C., Willand, N., Deprez, B., & Deprez-Poulain, R. A versatile solid-phase synthesis of 3-aryl-1,2,4-oxadiazolones and analogues. Tetrahedron Letters,2007, 48(8): 1479-1483. doi:10.1016/j.tetlet.2006.12.050

Deprez-Poulain, R. F., Charton, J., Leroux, V., & Deprez, B. P. Convenient synthesis of 4H-1,2,4-triazole-3-thiols using di-2-pyridylthionocarbonate. Tetrahedron Letters,2007, 48(46): 8157-8162. doi:10.1016/j.tetlet.2007.09.094

Dubs, P., Bourel-Bonnet, L., Subra, G., Blanpain, A., Melnyk, O., Pinel, A. M., Gras-Masse, H., & Martinez, J.
Parallel synthesis of a lipopeptide library by hydrazone-based chemical ligation. J Comb Chem,2007, 9(6): 973-981.
doi: 10.1021/cc070033b

Flipo, M., Beghyn, T., Charton, J., Leroux, V. A., Deprez, B. P., & Deprez-Poulain, R. F. A library of novel hydroxamic acids targeting the metallo-protease family: design, parallel synthesis and screening. Bioorganic and Medicinal Chemistry,2007, 15(1): 63-76. doi:10.1016/j.bmc.2006.10.010

Flipo, M., Beghyn, T., Leroux, V., Florent, I., Deprez, B. P., & Deprez-Poulain, R. F. Novel Selective Inhibitors of the Zinc Plasmodial Aminopeptidase PfA-M1 as Potential Antimalarial Agents. Journal of Medicinal Chemistry,2007, 50(6): 1322-1334.

Gras-Masse, H., & Willand, N. Neuraminidase inhibitors and risk of H5N1 influenza. Annales Pharmaceutiques Francaises,2007, 65(1): 50-57.

Host, H., Drobecq, H., Locht, C., & Menozzi, F. D. Enzymatic methylation of the Mycobacterium tuberculosis heparin-binding haemagglutinin. FEMS Microbiology Letters,2007, 268(2): 144-150. doi:10.1111/j.1574-6968.2007.00 6.x

Willand, N., Folléas, B., Boutillon, C., Verbraeken, L., Gesquiere, J.-C., Tartar, A., & Deprez, B. Efficient, Two-Step Synthesis O N-Substituted Nortropinone Derivatives. Tetrahedron Letters,2007, 48(29): 5007-5011.doi:10.1016/j.tetlet.2007.05.110

Beghyn, T.; Hounsou, C.; Deprez, B. P., PDE5 inhibitors: An original access to novel potent arylated analogues of tadalafil.
Bioorg. Med. Chem. Lett. 2007, 17, (3), 789-92.doi:10.1016/j.bmcl.2006.10.069

Deprez, B. 2007. Le criblage à haut contenu d'information pour la génétique chimique directe (criblage phénotypique sur organismes) et inverse (cribl e structural par RMN). In E. Marechal, S. Roy, & F. Lafanechere (Eds.), Chemogénomique: Des petites molécules pour explorer le vivant: 109-119: EDP Sciences.


Ashworth, D. M., Batt, A. R., Baxter, A. J., Broqua, P., Haigh, R., M., Hudson, P., Heeney, C. M. S., Laporte, R., Penson, A., Pitt, G. R. W., Robson, P. A., Rooker, D. P., Tartar, A. L., Ye C. M., & Roe, M. B.
Nonpeptide oxytocin agonists.
Drugs of the Future,2006, 31(4): 345-353.

Charton, J., Girault-Mizzi, S., Debreu-Fontaine, M.-A., Foufelle, F., Hainault, I., Bizot-Espiard, J.-G., Caignard, D.-H., & Sergheraert, C. Synthesis and biological evaluation of benzimidazole derivatives as potent AMP-activated protein kinase activators. Bioorganic & Medicinal Chemistry,2006, 14(13): 4490. doi:10.1016/j.bmc.2006.02.028

Deprez-Poulain, R., & Deprez, B. Trends in Hit-to-Lead: An Update. Frontiers in Medicinal Chemistry,2006, 3(1): 653-673.

Melnyk, P., Leroux, V., Sergheraert, C., & Grellier, P. Design, synthesis and in vitro antimalarial activity of an acylhydrazone library. Bioorg Med Chem Lett.,2006, 16(1): 31-35. doi:10.1016/j.bmcl.2005.09.058

Toto, P., Gesquiere, J.-C., Cousaert, N., Deprez, B., & Willand, N. UFU (Ullmann-Finkelstein-Ullmann): a new multicomponent reaction. Tetrahedron Letters,2006, 47(28): 4973-4978. doi:10.1016/j.tetlet.2006.04.041

Toto, P., Gesquiere, J.-C., Deprez, B., & Willand, N. Synthesis of N-(iodophenyl)-amides via an unprecedented Ullmann-Finkelstein tandem reaction. Tetrahedron Letters,2006, 47(7): 1181-1186.doi:10.1016/j.tetlet.2005.12.022

Villefroy, P., Letourneur, F., Coutsinos, Z., Mortara, L., Beyer, C., Gras-Masse, H., Guillet, J. G., & Bourgault-Villada, I.
SIV escape mutants in rhesus macaques vaccinated with NEF-derived lipopeptides and challenged with pathogenic SIVmac251. Virol J,2006, 3: 65.


Caroline Smet, Jean-Frédéric Duckert, Jean-Michel Wieruszeski, Isabelle Landrieu, Luc Buée, Guy Lippens, and Benoît Déprez.
Control of protein-protein interactions: structure-based discovery of low molecular weight inhibitors of the interactions between Pin1 WW domain and phosphopeptides. J.Med.Chem , 2005, 48, (15), 4815-4823

Nicolas Cousaert, Patrick Toto, Nicolas Willand, and Benoît Déprez. Efficient, Protection-Free Suzuki-Miyaura Synthesis of ortho-biphenyltetrazoles. Tet Let, 2005, 46, 6529-6532.

Jolimaitre, P., Roux, A., Blanpain, A. , Leduc, C., Bassereau, P., Bourel-Bonnet, L. Synthesis and pre inary physical applications of a rhodamin-biotin phosphatidylethanolamine, an easy attainable lipid double probe Chem Phys Lipids, 2005, 133, (2), 215-23

Déprez-Poulain R, Melnyk P. Libraries of 1,4-bis(aminopropyl)piperazine antimalarials : from discovery to the coming generation. Comb. Chem. And High Through. Screen. Review, 2005, 8, (1), 39-48

Coutsinos, Z., Villefroy, P., Gras-Masse, H., Guillet, J. G., Bourgault-Villada, I. Evaluation of SIV-lipopeptide immunizations administered by the intradermal route in their ability to induce antigen specific T-cell responses in rhesus macaques
FEMS Immunol Med Microbiol, 2005, 43, (3), 357-66

Bourel-Bonnet, L., Rao, K. V., Hamann, M. T., Ganesan, A. Solid-phase total synthesis of kahalalide A and related analogues
J Med Chem, 2005, 48, 5, 1330-5

Bourel-Bonnet, L., Pecheur, E. I., Grandjean, C., Blanpain, A., Baust, T., Melnyk, O., Hoflack, B., Gras-Masse, H.
Anchorage of synthetic peptides onto liposomes via hydrazone and alpha-oxo hydrazone bonds. preliminary functional investigations Bioconjug Chem, 2005, 16, 2, 450-7


Pitt G, Batt A, Haigh R, Penson A, Robson P, Rooker D, Tartar A, Trim J, Yea C, Roe M. Non-peptide oxytocin agonists.
Biorg. & Med. Chem. Lett. 2004, 6 sept.; 14 (17): 4585-4589.

Déprez-Poulain R, Melnyk P. Libraries of 1,4-bis(aminopropyl)piperazine antimalarials : from discovery to the coming generation. Comb. Chem. And High Through. Screen.

Déprez-Poulain R, Willand N, Boutillon C, Nowogrocki G, Azaroual N, Déprez B. A simple reaction to produce small structurally complex and diverse molecules. Tetrahedron Lett. 2004; 45 (27): 5287-5290.

Willand N, Beghyn T, Nowogrocki G, Gesquière J-C, Déprez B. Synthesis and structural studies of a novel scaffold for drug discovery: a 4,5-dihydro-3 H-spiro[1,5-benzoxazepine-2,4 '-piperidine]. Tetrahedron Lett. 2004; 45 (5): 1051-1054.

Déprez-Poulain R, Déprez B. Facts, Figures and Trends in Lead Generation. Current Topics in Medicinal Chemistry 2004; 4 (6): 569-580.

Guillon J, Grellier P, Labaied M, Léger J-M, Sonnet P, Déprez-Poulain R, Dallemagne P, Lemaître N, Rault S, Rochette J, Sergheraert C, Jarry C. Synthesis, Antimalarial Activity and Cytotoxicity of New Pyrrolo[1,2-a]quinoxalines, Bispyrrolo[1,2-a]quinoxalines, Bispyrido[3,2-e]pyrrolo[1,2-a]pyrazines and Bispyrrolo[1,2-a]thieno[3,2-e]pyrazine J. Med. Chem. 2004; 47(8): 1997-2009.

Charton J, Cazenave Gassiot A, Girault-Mizzi S, Melnyk P, Sergheraert C. Optimized Synthesis of Tetrahydroisoquinoline-Hydantoins. Tetrahedron Lett. 2004; 45: 7081-7085.

Duburcq X, Olivier C, Malingue F, Desmet R, uzidi A, Z u F, Auriault C, Gras-Masse H, Melnyk O. Peptide-protein microarrays for the simultaneous detection of pathogen infections. Bioconjugate Chem. 2004; 15(2): 307-316.


Bourel-Bonnet L, Bonnet D, Malingue F, Gras-Masse H, Melnyk O. Simultaneous Lipidation of a Characterized Peptide Mixture by Chemoselective Ligation. Bioconj. Chem. 2003; 2: 494-499.

Bonnet D, Grandjean C, Rousselot-P ley P, Joly P, Bourel-Bonnet L, Santrai V, Gras-Masse H, Melnyk O. Solution Phase Functionalization of Peptides by an alpha-hydrazinoacetyl group. J. Org. Chem. 2003; 68: 7033-40.

Chenevier P, Bourel-Bonnet L, Roux D. Chemical characterization of alpha-oxo hydrazone ligation on colloids: toward grafting molecular addresses onto biological vectors. J. Am. Chem. Soc. 2003; 125: 16261-16270.

Flipo M, Florent I, Grellier P, Sergheraert C, Déprez-Poulain R. Design, synthesis and antimalarial activity of novel, quinolinebased, zinc metallo-aminopeptidase inhibitors. Bioorg.Med. Chem.Lett. 2003; 13: 2659-2662.

Ryckebusch A, Deprez-Poulain R, Maes L, Debreu-Fontaine M-A, Mouray E, Grellier P, Sergheraert C. Synthesis and in Vitro and in Vivo Antimalarial Activity of N1-(7-Chloro-4-quinolyl)-1,4-bis(3-aminopropyl)piperazine Derivatives. J. Med. Chem 2003; 46: 542-557.

Ryckebusch A, Deprez-Poulain R, Debreu-Fontaine M-A, Vandaele R, Mouray E, Grellier P, Sergheraert C.
Synthesis and Antimalarial Evaluation of New 1,4-bis(3-aminopropyl)piperazine Derivatives. Bioorg. Med. Chem. Lett. 2003; 13: 3783-3787.

Olivier C, Hot D, Huot L, Ollivier N, El-Mahdi O, Gouyette C, Huynh-Dinh T, Gras-Masse H, Lemoine Y, Melnyk O.
Alpha-Oxo Semicarbazone Peptide or Oligodeoxynucleotide Microarrays. Bioconjugate Chem. 2003 ; 14(2): 430-439.

Gras-Masse H. Lipid vector for the delivery of peptides towards intracellular pharmacological targets. J. Mol. Recognit. 2003 16(5): 234-239.

Gahery-Segard H, Pialoux G, Figueiredo S, Igea C, Surenaud M, Gaston J, Gras-Masse H, Levy JP, Guillet JG. Long-term specific immune responses induced in humans by human immunodeficiency virus type 1 lipopeptide vaccine: characterization of CD8+-T-cell epitopes recognized. J. Virol. 2003; 77(20): 11220-11231.

BenMohamed L, Bertrand G, McNamara CD, Gras-Masse H, Hammer J, Wechsler SL, Nesburn AB Identification of novel immunodominant CD4+ Th1-type T-cell peptide epitopes from herpes simplex virus glycoprotein D that confer protective immunity. J. Virol. 2003; 77(17): 9463-9473.

Crochley P, Willand N, Rullay A.K, Crout D.H.G. Carbohydrate-protein interactions at interfaces: synthesis of thiolactosyl glycolipids and design of a working model for surface plasmon resonance. Organic & Biomolecular Chemistry 2003; 1(6): pages 928-938.


Willand N, Joossens J, Gesquière J-C, Tartar A.L, Evans M, Roe M.B.
Solid and sol ion phase syntheses of the 2-cyanopyrrolidide DPP-IV inhibitor NVP-DPP728. Tetrahedron 2002; 58(28): 5741-5746.

Ryckebusch A, Déprez-Poulain R, Debreu-Fontaine M-A, Vandaele R, Mouray E, Grellier P,
Sergheraert C.
Parallel Synthesis and Anti-Malarial Activity of a Sulfonamide Library.
Bioorg. Med. Chem. Lett. 2002; 12: 2595-2598.

Chenevier P, Grandjean C, Loing E, Malingue F, Angyalosi G, Gras-Masse H, Roux D, Melnyk O, Bourel-Bonnet L.
Grafting of synthetic mannose receptor-ligands onto onion vectors for the human dendritic cells' targeting.
Chem. Commun. 2002; 20: 2446-2447.

Fruchart JS, Lippens G, Kuhn C, Gras-Masse H, Melnyk O.
Solid-phase enolate chemistry investigated using HR-MAS NMR spectroscopy
J. Org. Chem. 2002; 67: 526-532.

Ollivier N, Olivier C, Gouyette G, Tam HD, Gras-Masse H, Melnyk O.
Synthesis of oligonucleotide-peptide conjugates using hydrazone chemical ligation
Tetrahedron Lett. 2002; 43: 997-999.

Urbès F, Fruchart JS, Gras-Masse H, Melnyk O.
C-terminal glyoxylyl peptides for sensitive enzyme-linked immunosorbent assays.
Lett. in Pept. Sci. 2002; 8: 253-258.

Angyalosi G, Grandjean C, Lamirand M, Auriault C, Gras-Masse H, Melnyk O.
Synthesis and mannose receptor-Mediated uptake of clustered glycomimetics by human dendritic cells: effect of charge.
Bioorg. Med. Chem. Lett. 2002; 12(19): 2723-2727.

BenMohamed L, Belkaid Y, Loing E, Brahimi K, Gras-Masse H, Druilhe P.
Systemic immune responses induced by mucosal administration of lipopeptides without adjuvant.
Eur. J. Immunol. 2002; 32(8): 2274-2281.

Banic DM, Goldberg AC, Pratt-Riccio LR, De Oliveira-Ferreira J, Santos F, Gras-Masse H, Camus D, Kalil J, Daniel-Ribeiro CT.
Human leukocyte antigen class II control of the immune response to p126-derived amino terminal peptide from Plasmodium falciparum.
Am. J. Trop. Med. Hyg. 2002; 66(5): 509-515.

Grandjean C, Santraine V, Fruchart JS, Melnyk O, Gras-Masse H.
Combined thioether/hydrazone chemoselective ligation reactions for the synthesis of glycocluster-antigen Peptide conjugates.
Bioconjugate Chem. 2002; 13(4): 887-892.

Melnyk O, Duburcq X, Olivier C, Urbes F, Auriault C, Gras-Masse H.
Peptide arrays for highly sensitive and specific antibody-binding fluorescence assays.
Bioconjugate Chem. 2002; 13(4): 713-720.

Le Gal FA, Prevost-Blondel A, Lengagne R, Bossus M, Farace F, Chaboissier A, Gras-Masse H, Engelhard VH, Guillet JG, Gahery-Segard H.
Lipopeptide-bas lanoma cancer vaccine induced a strong MART-27-35-cytotoxic T lymphocyte response in a preclinal study.
Int. J. Cancer 2002; 98(2): 221-227.


Pialoux G, Ségard H, Sermet S, Poncelet H, Fournier S, Gerard L, Tartar A, Gras-Masse H, Levy J-P, Guillet J-C.
Lipopetides induce cell-mediated anti-HIV immune responses in seronegative volunteers.
AIDS, 2001; 15: 1239-1249.

Bourel-Bonnet L, Gras-Masse H, Melnyk O.
A Novel Family of Amphiphilic a -oxo aldehydes for the Site-specific Modification of Peptides by two Palmitoyl groups in Solution or in Liposome Suspension.
Tetrahedron Lett. .2001; 42: 6851-6853.

Poulain R.F, Horvath D, Bonnet B, Eckhoff C, Chapelain B, Bodinier M-C, Déprez B.
From Hit to Lead: Combining two Complementary Methods for Focused Library Design. Application to µ opiate Ligands.
J. Med. Chem. 2001; 44(21): 3378-3390.

Poulain R.F, Horvath D, Bonnet B, Eckhoff C, Chapelain B, Bodinier M-C, Déprez B.
From Hit to Lead: Analyzing Structure-Profile Relationships.
J. Med. Chem. 2001; 44(21): 3391-3401.

Poulain R, Tartar A, Déprez B.
Parallel Synthesis of 1,2,4-oxadiazoles from carboxylic acids using an improved, uronium-based, activation. Tetrahedron Lett. 2001; 42: 1495-1498.

Charton J, Delarue S, Vendeville S, Debreu-Fontaine M-A, Girault-Mizzi S, Sergheraert S.
Convenient synthesis of tetrahydroisoquinoline-hydantoins.
Tetrahedron Lett. 2001; 42: 7559-7561.

Grandjean C, Gras-Masse H, Melnyk O.
Synthesis of clustered glycoside-antigen conjugates by two one-pot, orthogonal, chemoselective ligation reactions: scope and limitations.
Chemistry, a Eur. J. 2001; 1: 230-239.

Bonnet D, Thiam K, Loing E, Melnyk O, Gras-Masse H.
Synthesis by Chemoselective Ligation and Biological Evaluation of Novel Cell-permeable PKC-zeta Pseudosubstrate Lipopeptides.
J. Med. Chem. 2001; 44: 468-471.

Bonnet D, Ollivier N, Gras-Masse H, Melnyk O.
Chemoselective acylation of fully deprotected hydrazino acetyl peptides. application to the synthesis of lipopeptides.
J. Org. Chem. 2001; 66: 443-449.

Bonnet D, Joly P, Gras-Masse H, Melnyk O.
Synthesis of an amphiphilic aldehyde by using as a key step the condensation of a lipophilic glyoxylic acid amide derivative with tris (hydroxymethyl) aminomethane.
Tetrahedron Lett. 2001; 42: 1875-1877.

Melnyk O, Fruchart JS, Grandjean C, Gras-Masse H.
A tartric acid-based linker for the solid phase synthesis of C-terminal peptide alpha-oxo aldehydes.
J. Org. Chem. 2001; 66: 4153-4160.

Pialoux G, Gahery-Segard H, Sermet S, Poncelet H, Fournier S, Gérard L, Tartar A, Gras-Masse H, Levy JP, Guillet JG.
Lipopeptides induce cell-mediated anti-HIV immune responses in seronegative volunteers. The ANRS VAC04 trial. r />AIDS, 001; 15: 1239-1249.

Grandjean C, Angyalosi G, Loing E, Adriannssens E, Melnyk O, Pancré V, Auriault C, Gras-Masse H
Novel Hyper-Branched Designed Glycomimetics Recognized by the Human Mannose Receptor: Quinic or Shikimic amides as Mannose Bioisosteres.
Chem. Biochem. 2001; 2: 747-757.

Gras-Masse H.
Chemoselective Ligation and Antigen vectorization. Developments in Biologicals. International Association for Biologicals.
Biologicals 0 29: 183-188.

Eckenberg R, Ro T, Moreau JL, Weil R, Gesbert F, Dubois S, Tello D, Bossus M, Gras-Masse H, Tartar A, Bertoglio J, Chouaïb S, Jacques Y, Alzari P, Thèze J.
Characerization of an IL-2 mimetic with therapeutic potential.
Cellular and Molecular Biology 2001; 47(4): 703-707.

Duez C, Gras-Masse H, Hammad H, Akoum H, Didierlaurent A, André C, Tonnel AB, Pestel J.
Modulation of the allergen-induced human IgE response in Hu-SCID mice : inhibitory effect of human recombinant IFN-g and allergen-derived lipopeptide.
Eur. Cytokine New 2001; 13 (3) : 453-461.

Gras-Masse H.
Single-chain lipopeptide vaccines for the induction of virus-specific cytotoxic T cell responses in randomly selected populations.
Molecular Immunol. 2001; 38: 423-431.

Fruchart JS, Gras-Masse H, Melnyk O.
Methyl phenylacetate enolate generated with P4-tBu Schwesinger base: naked" or not?
Tetrahedron Lett. 2001; 42: 9153-9155.

Hosmalin A, Andrieu M, Loing E Desoutter JF, Hanau D, Gras-Masse H, Dautry-Varsat A, Guillet JG.
Lipopeptide presentation pathway in dendritic cells.
Immunol. Lett., 2001, 79, 1-2 : 97-100.


Klingueur C., David D., Kouach M., Wieruszeski J.M., Tartar A., Marzin D., Levy J.P., Gras-masse H.
Characterization of a multi-lipopeptides mixture used as an HIV-1 vaccine candidate.
Vaccine, 2000, 18, 259-267.

Ségard H, Pialoux G, Charmetau B, Sermet S, Poncelet H, Raux M, Tartar A, Levy J-P, G s-Masse H, Guillet J-C.
Multiepitopic B- and T-Cell responses induced in humans by a human Immunodeficiency virus type 1 lipopetide vaccine.
Journal of Virology, 2000; 74: 1694-1703. r />
Salmon-Chemin L, Lemaire A, De Freitas S, Déprez B, Sergheraert C, Davioud Charvet E.
Parallel Synthesis of a Library of 1,4 Naphtoquinones and Automated Screening of Potential Inhibitors of Trypanothione Reductase from Trypanosoma cruzi.
Bioorg. Med. Chem. Lett. 2000; 10: 631-635.

Yu N, Poulain R, Gesquière J-C.
A One-Pot Synthesis of Tetrahydroisoquinolonic Acids from Aldehydes and Amines in trimethylorth ormate.
Syn. Lett. 2000; 3: 349-350.

Tartar A, Poulain R.F.
La Chimie Combinatoire, La Science au Présent 2001.
Encyclopeaedia Universalis, 2000 ; 114-119.

Bourel L, Carion O, Gras-Masse H, Melnyk O.
The deprotection of Lys(Mtt) revisited.
J. Pept. Sci. 2000 ; 6 : 264-270.

Bonnet D, Bourel L, Gras-Masse H, Melnyk O.
A Novel Lipophilic Glyoxylic Acid Deriva ve for the Lipidation of Peptides using Salt-free Ligation. Tetrahedron Lett. 2000; 41: 10003-10007.

Loing E, Thiam K, Andrieu M, Schörner D, Wiesmüller KH, Hosmalin A, Jung G, Gras-Masse H.
Modification of an HLA-A*0201-retricted Minimal Cytotoxic Epitope by an Additionnal Palmitoyl-Lysine Residue Increases the Life Span of Functionnal Presentation to Wild-Type Specific Cytotoxic T Cells.
J. Immunol. 2000; 164: 900-907.

Gahéry-Ségard H, Pialoux G, Charmeteau B, Sermet S, Poncelet H, Raux M, Tartar A, Lévy JP, Gras-Masse H, Guillet